Sekimata, Katsuhiko; Sato, Tomohiro; Sakai, Naoki; Watanabe, Hisami; Mishima-Tsumagari, Chiemi; Taguri, Tomonori; Matsumoto, Takehisa; Fujii, Yoshifumi; Handa, Noriko; Honma, Teruki; Tanaka, Akiko; Shirouzu, Mikako; Yokoyama, Shigeyuki; Miyazono, Kohei; Hashizume, Yoshinobu; Koyama, Hiroo published the artcile< Bis-heteroaryl pyrazoles: identification of orally bioavailable inhibitors of activin receptor-like kinase-2 (R206H)>, HPLC of Formula: 93-60-7, the main research area is bisheteroaryl pyrazole ALK2 mutation inhibitor oral bioavailability; activin receptor-like kinase-2; fibrodysplasia ossificans progressiva; inhibitor.
Mutant activin receptor-like kinase-2 (ALK2) was reported to be closely associated with the pathogenesis of fibrodysplasia ossificans progressiva (FOP) and diffuse intrinsic pontine glioma (DIPG), and therefore presents an attractive target for therapeutic intervention. Through in silico virtual screenings and structure-activity relationship studies assisted by X-ray crystallog. analyses, a novel series of bis-heteroaryl pyrazole was identified as potent inhibitors of ALK2 (R206H). Derived from in silico hit compound RK-59638 (6a), compound 18p was identified as a potent inhibitor of ALK2 (R206H) with good aqueous solubility, liver microsomal stability, and oral bioavailability.
Chemical & Pharmaceutical Bulletin published new progress about Activin receptor ACVRLK2 Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 93-60-7 belongs to class pyridine-derivatives, and the molecular formula is C7H7NO2, HPLC of Formula: 93-60-7.